scholarly journals Metabolic Profiling of the Soft Coral Erythropodium caribaeorum (Alcyonacea: Anthothelidae) from the Colombian Caribbean Reveals Different Chemotypes

Marine Drugs ◽  
2019 ◽  
Vol 18 (1) ◽  
pp. 4 ◽  
Author(s):  
Sandra L. Molina ◽  
Abel M. Forero ◽  
Farja I. Ayala ◽  
Mónica Puyana ◽  
Sven Zea ◽  
...  
Keyword(s):  
Soft Coral ◽  
Human Cancer ◽  
Principal Component ◽  
Caribbean Sea ◽  
Chemical Diversity ◽  
Human Cancer Cell Lines ◽  
Low Diversity ◽  
Ic50 Values ◽  
The Caribbean ◽  
Erythropodium Caribaeorum

The Caribbean soft coral Erythropodium caribaeorum is a rich source of erythrolides—chlorinated briarane diterpenoids. These compounds have an ecological role as feeding deterrents, with a wide variation in their composition depending on the location where the sample is collected. In Colombia, this soft coral can be found at different locations in the Caribbean Sea including Santa Marta, Islas del Rosario, and Providencia—three environmentally different coral reef areas in the south and southwest Caribbean Sea. In order to evaluate differences in erythrolide composition, the metabolic profiles of samples from each of these locations were analyzed by HPLC-MS. Principal component analysis showed changes in the diterpene composition according to the sample origin. Diterpenes from samples collected at each location were isolated to describe the three chemotypes. The chemotype from Santa Marta was highly diverse, with the new erythrolides W and X together with eight known erythrolides. The sample from Islas del Rosario showed a low diversity chemotype constituted by high amounts of erythrolide A and B. The chemotype from Providencia showed low chemical diversity with only two main compounds—erythrolide V and R. Evaluation of cytotoxic activity against the human cancer cell lines PC-3, MCF7, and A549 showed erythrolides A and B as the more active compounds with IC50 values in the range from 2.45 to 30 μM.

scholarly journals Pipecolisporin, a Novel Cyclic Peptide with Antimalarial and Antitrypanosome Activities from a Wheat Endophytic Nigrospora oryzae

2021 ◽  
Vol 14 (3) ◽  
pp. 268
Author(s):  
Ignacio Fernández-Pastor ◽  
Victor González-Menéndez ◽  
Frederick Annang ◽  
Clara Toro ◽  
Thomas A. Mackenzie ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Agricultural Land ◽  
Cyclic Peptide ◽  
Human Cancer ◽  
Fungal Endophyte ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Micromolar Range ◽  
Nigrospora Oryzae

A novel cyclic antimalarial and antitrypanosome hexapeptide, pipecolisporin (1), was isolated from cultures of Nigrospora oryzae CF-298113, a fungal endophyte isolated from roots of Triticum sp. collected in a traditional agricultural land of Montefrío, Granada, Spain. The structure of this compound, including its absolute configuration, was elucidated by HRMS, 1-D and 2-D NMR spectroscopy, and Marfey’s analysis. This metabolite displayed interesting activity against Plasmodium falciparum and Trypanosoma cruzi, with IC50 values in the micromolar range, and no significant cytotoxicity against the human cancer cell lines A549, A2058, MCF7, MIA PaCa-2, and HepG2.

Six New neo-Clerodane Diterpenoids from Aerial Parts of Scutellaria barbata and Their Cytotoxic Activities

Planta Medica ◽  
2018 ◽  
Vol 84 (17) ◽  
pp. 1292-1299 ◽  
Author(s):  
Guo-Chun Yang ◽  
Jia-Hui Hu ◽  
Bing-Long Li ◽  
Huan Liu ◽  
Jia-Yue Wang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Scutellaria Barbata ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Clerodane Diterpenoids

AbstractSix new neo-clerodane diterpenoids (1–6), scutebatas X – Z, A1-C1, along with twelve known ones (7–18) were obtained via the phytochemical investigation of the aerial parts of Scutellaria barbata. Their structures were established by detailed spectroscopic analysis. The absolute configurations of 1 and 2, as the representative members of this type, were identified based on a circular dichroic exciton chirality method. Moreover, in vitro cytotoxicity of compounds 1–6 were evaluated against three human cancer cell lines (SGC-7901, MCF-7, and A-549) using the MTT method. Compound 6 showed cytotoxic activities against all the three cell lines with IC50 values of 17.9, 29.9, and 35.7 µM, respectively.

scholarly journals Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 437
Author(s):  
Shu-Qin Qin ◽  
Lian-Chun Li ◽  
Jing-Ru Song ◽  
Hai-Yun Li ◽  
Dian-Peng Li
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
A549 Cells ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Diphenyl Tetrazolium Bromide ◽  
Conjugated Compounds

A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 μM.

scholarly journals Triangulene C, A New Cubitane-Based Diterpenoid from the Soft Coral Sinularia Triangula

2012 ◽  
Vol 7 (4) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Huey-Jen Su ◽  
Nai-Lun Lee ◽  
Mei-Chin Lu ◽  
Jui-Hsin Su
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Data ◽  
Soft Coral ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Hct 116

A new cubitane-based diterpenoid, triangulene C (1), was isolated from the soft coral Sinularia triangula and its structure was elucidated on the basis of spectroscopic data. Compound 1 was not cytotoxic (IC50 >20 μg/mL) toward the four human cancer cell lines tested (HL60, MDA-MB-231, HCT-116 and DLD-1).

scholarly journals Cytotoxic Polyketides from the Marine Sponge-Derived Fungus Pestalotiopsis heterocornis XWS03F09

Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2655 ◽  
Author(s):  
Lei ◽  
Lei ◽  
Zhou ◽  
Hu ◽  
Niu ◽  
...  
Keyword(s):  
Marine Sponge ◽  
Spectroscopic Analysis ◽  
Fermentation Broth ◽  
Human Cancer ◽  
Optical Rotation ◽  
Cytotoxic Activities ◽  
Human Cancer Cell Lines ◽  
Chemical Structures ◽  
Ic50 Values ◽  
New Compounds

Four new compounds, including two new polyketides, heterocornols M and N (1, 2), and a pair of epimers, heterocornols O and P (3, 4), were isolated from the fermentation broth of the marine sponge-derived fungus Pestalotiopsis heterocornis XWS03F09, together with three known compounds (5–7). The new chemical structures were established on the basis of a spectroscopic analysis, optical rotation, experimental and calculated electronic circular dichroism (ECD). All of the compounds (1–7) were evaluated for their cytotoxic activities, and heterocornols M-P (1–4) exhibited cytotoxicities against four human cancer cell lines with IC50 values of 20.4–94.2 μM.

scholarly journals Four New ent-Kaurane Diterpene Glycosides from Isodon henryi

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2736 ◽  
Author(s):  
Liu ◽  
Zhang ◽  
Wu ◽  
Chen ◽  
Li ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Spectroscopic Methods ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Hct 116 ◽  
Relationship Of ◽  
First Time

To obtain diterpene glycosides from an aqueous extract of the aerial parts of Isodon henryi and further investigate their cytotoxicities, in this study, a total of seven compounds were isolated, including six ent-kaurane diterpene glycosides (1–6) and one diterpene aglycon (7). Among the seven ent-kaurane diterpenes obtained, four were novel compounds, including ent-7,20-epoxy- kaur-16-en-1α,6β,7β,15β-tetrahydroxyl-11-O-β-d-glucopyranoside (1), ent-7,20-epoxy-kaur-16-en- 6β,7β,14β,15β-tetrahydroxyl-1-O-β-d-glucopyranoside (2), ent-7,20-epoxy-kaur-16-en-6β,7β,15β- trihydroxyl-1-O-β-d-glucopyranoside (3), and ent-7,20-epoxy-kaur-16-en-7β,11β,14α,15β-tetrahydr- oxyl-6-O-β-d-glucopyranoside (4), and three were isolated from this plant for the first time (5–7). Their structures were elucidated by utilizing spectroscopic methods and electronic circular dichroism analyses. Furthermore, the cytotoxicities of all seven compounds were investigated in four human cancer cell lines, including A2780, BGC-823, HCT-116, and HepG2. The IC50 values of these diterpenes ranged from 0.18 to 2.44 mM in the tested cell lines. In addition, the structure–cytotoxicity relationship of diterpene glycosides was also evaluated to study the effect of glycosylation on the cytotoxicity of diterpene compounds.

Barringtogenol C-type Triterpenoid Saponins from the Stem Bark of Norway Maple (Acer Platanoides)

Planta Medica ◽  
2019 ◽  
Vol 86 (01) ◽  
pp. 70-77 ◽  
Author(s):  
Wen Xu ◽  
Lu Zhang ◽  
Raed Omar ◽  
Wei Liu ◽  
Zhengxi Wei ◽  
...  
Keyword(s):  
Human Cancer ◽  
Stem Bark ◽  
Acer Platanoides ◽  
Human Cancer Cell ◽  
Triterpenoid Saponins ◽  
Human Cancer Cell Lines ◽  
Spectroscopic Analyses ◽  
Chemical Hydrolysis ◽  
Norway Maple ◽  
Ic50 Values

AbstractFour new barringtogenol C-type triterpenoid saponins, namely acerplatanosides A – D (1–4), along with 22 known compounds (5–26), were isolated from the stem bark of Norway maple (Acer platanoides). Their structures were elucidated on the basis of comprehensive spectroscopic analyses and chemical hydrolysis. This is the first report of triterpenoid saponins isolated from Norway maple. Compounds 1, 3, and 4 showed cytotoxicity against 4 human cancer cell lines with IC50 values ranging from 9.4 to 39.5 µM.

scholarly journals Chemical constituents and cytotoxicity of Aspidistra letreae

2020 ◽  
Vol 129 (1B) ◽  
pp. 31-39
Author(s):  
Duc Viet Ho ◽  
Hanh Nhu Thi Hoang ◽  
Khue Minh Vo ◽  
Anh Tuan Le ◽  
Hoai Thi Nguyen
Keyword(s):  
Human Cancer ◽  
Chemical Constituents ◽  
Hep G2 ◽  
Human Cancer Cell Lines ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
Reported Data ◽  
Whole Plants ◽  
First Time

A phytochemical investigation of whole Aspidistra letreae plants led to the isolation of 2H-chromen-2-one (1), α-tocopherol (2), (E)-phytol (3), asparenydiol (4) and (25S)-spirost-1β,3α,5β-triol (5). Their structures were determined on the basis of NMR spectral evidences and in comparison with the reported data. Of these, asparenydiol (4) was isolated from the genus Aspidistra for the first time. This is also the first report on the separation and structural determination of (25S)-spirost-1β,3α,5β-triol (5) as a pure compound. The methanol extract from the whole plants of Aspidistra letreae exhibits moderate cytotoxicity against the LU-1, HeLa, MDA-MB-231, Hep-G2, and MKN-7 human cancer cell lines with IC50 values ranging from 52.58 ± 3.65 to 64.78 ± 4.89 μg/mL.

scholarly journals Cyclodepsipeptides and Sesquiterpenes from Marine-Derived Fungus Trichothecium roseum and Their Biological Functions

Marine Drugs ◽  
2018 ◽  
Vol 16 (12) ◽  
pp. 519 ◽  
Author(s):  
Yuan-Ming Zhou ◽  
Guang-Lin Ju ◽  
Lin Xiao ◽  
Xiang-Fei Zhang ◽  
Feng-Yu Du
Keyword(s):  
Brine Shrimp ◽  
Human Cancer ◽  
Crystallographic Analysis ◽  
Heterodera Avenae ◽  
Cytotoxic Activities ◽  
Brine Shrimp Lethality ◽  
Human Cancer Cell Lines ◽  
Trichothecium Roseum ◽  
Ic50 Values ◽  
Ld50 Value

On the basis of the ‘one strain, many compounds’ (OSMAC) strategy, chemical investigation of the marine-derived fungus Trichothecium roseum resulted in the isolation of trichomide cyclodepsipeptides (compounds 1–4) from PDB medium, and destruxin cyclodepsipeptides (compounds 5–7) and cyclonerodiol sesquiterpenes (compounds 8–10) from rice medium. The structures and absolute configurations of novel (compounds 1, 8, and 9) and known compounds were elucidated by extensive spectroscopic analyses, X-ray crystallographic analysis, and ECD calculations. All isolated compounds were evaluated for cytotoxic, nematicidal, and antifungal activities, as well as brine shrimp lethality. The novel compound 1 exhibited significant cytotoxic activities against the human cancer cell lines MCF-7, SW480, and HL-60, with IC50 values of 0.079, 0.107, and 0.149 μM, respectively. In addition, it also showed significant brine shrimp lethality, with an LD50 value of 0.48 μM, and moderate nematicidal activity against Heterodera avenae, with an LC50 value of 94.9 μg/mL. This study constitutes the first report on the cytotoxic and nematicidal potential of trichomide cyclodepsipeptides.

scholarly journals Fine-Tuning the Activation Mode of an 1,3-Indandione-Based Ruthenium(II)-Cymene Half-Sandwich Complex by Variation of Its Leaving Group

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2373 ◽  
Author(s):  
Stephan Mokesch ◽  
Daniela Schwarz ◽  
Michaela Hejl ◽  
Matthias H. M. Klose ◽  
Alexander Roller ◽  
...  
Keyword(s):  
Tumor Tissue ◽  
Human Cancer ◽  
Blood Stream ◽  
Fine Tuning ◽  
Minor Variation ◽  
Human Cancer Cell Lines ◽  
Leaving Group ◽  
Ic50 Values ◽  
The Stability ◽  
Ph Level

Fine-tuning of the properties of a recently reported 1,3-indandione-based organoruthenium complex is attempted to optimize the stability under physiological conditions. Previous work has shown its capacity of inhibiting topoisomerase IIα; however, fast aquation leads to undesired reactions and ligand cleavage in the blood stream before the tumor tissue is reached. Exchange of the chlorido ligand for six different N-donor ligands resulted in new analogs that were stable at pH 7.4 and 8.5. Only a lowered pH level, as encountered in the extracellular space of the tumor tissue, was capable of aquating the complexes. The 50% inhibitory concentration (IC50) values in three human cancer cell lines differed only slightly, and their dependence on the utilized leaving group was smaller than what would be expected from their differences in cellular accumulation, but in accordance with the very minor variation revealed in measurements of the complexes’ lipophilicity.

Sign in / Sign up

Export Citation Format

Share Document